Tìm theo
Ambenonium
Các tên gọi khác (3) :
  • Ambenonium
  • Ambenonium base
  • Ambenonum
Thuốc chống loạn nhịp
Thuốc Gốc
Small Molecule
CAS: 7648-98-8
ATC: N07AA30
ĐG : Bayer Healthcare , http://www.bayerhealthcare.com
CTHH: C28H42Cl2N4O2
PTK: 537.565
Ambenonium is a cholinesterase inhibitor used in the management of myasthenia gravis. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C28H42Cl2N4O2
Phân tử khối
537.565
Monoisotopic mass
536.268482022
InChI
InChI=1S/C28H40Cl2N4O2/c1-5-33(6-2,21-23-13-9-11-15-25(23)29)19-17-31-27(35)28(36)32-18-20-34(7-3,8-4)22-24-14-10-12-16-26(24)30/h9-16H,5-8,17-22H2,1-4H3/p+2
InChI Key
InChIKey=OMHBPUNFVFNHJK-UHFFFAOYSA-P
IUPAC Name
[(2-chlorophenyl)methyl](2-{[(2-{[(2-chlorophenyl)methyl]diethylazaniumyl}ethyl)carbamoyl]formamido}ethyl)diethylazanium
Traditional IUPAC Name
ambenonium
SMILES
CC[N+](CC)(CCNC(=O)C(=O)NCC[N+](CC)(CC)CC1=CC=CC=C1Cl)CC1=CC=CC=C1Cl
Độ tan chảy
196-199 °C
Độ hòa tan
Soluble
logP
-3.6
logS
-8.8
pKa (strongest acidic)
10.78
pKa (Strongest Basic)
-3.6
PSA
58.2 Å2
Refractivity
173.57 m3·mol-1
Polarizability
59.98 Å3
Rotatable Bond Count
15
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
2
Number of Rings
2
Bioavailability
0
Dược Lực Học : Ambenonium, similar to pyridostigmine and neostigmine, is used for the treatment of muscle weakness and fatigue in people with myasthenia gravis. It is postulated to exert its therapeutic effect by enhancing cholinergic function through the inhibition of the acetylcholine hydrolysis by acetylcholinesterase. Increased levels of acetylcholine has peripheral effects, as acetylcholine is also used in the brain, where it tends to cause excitatory actions. The glands that receive impulses from the parasympathetic part of the autonomic nervous system are also stimulated in the same way. This is why an increase in acetylcholine causes a decreased heart rate and increased production of saliva. Ambenonium is used less commonly than neostigmine or pyridostigmine but may be preferred in patients hypersensitive to the bromide ion. Ambenonium produces fewer muscarinic side effects than neostigmine, but more than pyridostigmine.
Cơ Chế Tác Dụng : Ambenonium is a cholinesterase inhibitor used in the management of myasthenia gravis. [Wikipedia] Ambenonium exerts its actions against myasthenia gravis by competitive, reversible inhibition of acetylcholinesterase. The disease myasthenia gravis occurs when the body inappropriately produces antibodies against acetylcholine receptors, and thus inhibits proper acetylcholine signal transmission (when acetylcholine binds to acetylcholine receptors of striated muscle fibers, it stimulates those fibers to contract). Ambenonium reversibly binds acetylcholinesterase at the anionic site, which results in the blockage of the site of acetycholine binding, thereby inhibiting acetylcholine hydrolysis and enhancing cholinergic function through the accumulation of acetycholine at cholinergic synpases. In turn this facilitates transmission of impulses across the myoneural junction and effectively treats the disease.
Dược Động Học :
▧ Absorption :
Oral - poorly absorbed from the gastrointestinal tract.
▧ Metabolism :
Plasma and hepatic
Độc Tính : LD50=150±44 mg/kg (orally in mice). Symptoms of overdose include muscle twitching, weakness and paralysis of voluntary muscles including the tongue, shoulders, neck and arms, blood pressure increase (with or without a slowing of heart rate), a sensation of internal trembling, severe anxiety, and panic. Death may occur rapidly if untreated.
Chỉ Định : Ambenonium is used to treat muscle weakness due to muscle disease (myasthenia gravis).
Tương Tác Thuốc :
  • Betamethasone The corticosteroid, betamethasone, may decrease the effect of the anticholinesterase, ambenonium.
  • Dexamethasone The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, ambenonium.
  • Fludrocortisone The corticosteroid, fludrocortisone, may decrease the effect of the anticholinesterase, ambenonium.
  • Hydrocortisone The corticosteroid, hydrocortisone, may decrease the effect of the anticholinesterase, ambenonium.
  • Prednisolone The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, ambenonium.
  • Prednisone The corticosteroid, prednisone, may decrease the effect of the anticholinesterase, ambenonium.
  • Tacrine The acetylcholinesterase inhibitor, Tacrine, may increase the adverse/toxic effects of Ambenonium, a cholinergic agonist. Monitor for increased cholinergic effects and toxicity.
  • Triamcinolone The corticosteroid, triamcinolone, may decrease the effect of the anticholinesterase, ambenonium.
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Mytelase 10 mg caplet
    Giá bán buôn : USD >1.86
    Đơn vị tính : caplet
  • Biệt dược thương mại : Mytelase 10 mg tablet
    Giá bán buôn : USD >1.86
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Mysuran
  • Công ty :
    Sản phẩm biệt dược : Mytelase
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01122
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2131
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508143
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07773
ChemSpider
http://www.chemspider.com/Chemical-Structure.2046.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0024-1287-04
PharmGKB
http://www.pharmgkb.org/drug/PA164764601
Wikipedia
http://en.wikipedia.org/wiki/Ambenonium
Drugs.com
http://www.drugs.com/cdi/ambenonium.html
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